VU0650786

Product Name: VU0650786
CAS No.: 1809085-30-0
Chemical Name: VU0650786
Synonyms: VU0650786;VU0650786, 10 mM in DMSO;(7R)-2-{[(5-chloropyridin-2-yl)oxy]methyl}-5-(2-fluoropyridin-3-yl)-7-methyl-4H,5H,6H,7H-pyrazolo[1,5-a]pyrazin-4-one;Pyrazolo[1,5-a]pyrazin-4(5H)-one, 2-[[(5-chloro-2-pyridinyl)oxy]methyl]-5-(2-fluoro-3-pyridinyl)-6,7-dihydro-7-methyl-, (7R)-;inhibit,anxiolytic activity,antidepressant,Inhibitor,VU-0650786,mGlu3 NAM,VU0650786,mGluR,Metabotropic glutamate receptors,VU 0650786
CBNumber: CB05419870
Molecular Formula: C18H15ClFN5O2
Formula Weight: 387.8
MOL File: 1809085-30-0.mol

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VU0650786 Property

Boiling point:: 587.4±50.0 °C(Predicted)
Density: 1.49±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : 250 mg/mL (644.66 mM);Water : < 0.1 mg/mL (insoluble)
form: Solid
pka: 0.99±0.22(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0030141
Product name: VU0650786
Purity: 99.97%
Packaging: 5mg
Price: $350
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: BRS0009223
Product name: VU-0650786
Purity: 95.00%
Packaging: 5MG
Price: $456.55
Updated: 2021/12/16

ChemScene

Product number: CS-0030141
Product name: VU0650786
Purity: 99.97%
Packaging: 10mg
Price: $500
Updated: 2021/12/16

ChemScene

Product number: CS-0030141
Product name: VU0650786
Purity: 99.97%
Packaging: 25mg
Price: $950
Updated: 2021/12/16

ChemScene

Product number: CS-0030141
Product name: VU0650786
Purity: 99.97%
Packaging: 50mg
Price: $1600
Updated: 2021/12/16

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VU0650786 Chemical Properties,Usage,Production

Uses

VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents[1].

in vivo

VU0650786 (VU786) (i.p., 30 mg/kg) increases the proportion of c-Fos-positive cells by approximately 4-fold, enhances synaptic strength in cone cell subpopulations, weakens thalamocortical long-term depression (LTD), and reduces passive coping in acute models of antidepressant-like activity in inducible cFos-EGFP mice^[2].
The pharmacokinetic parameters of VU0650786 (compound 106) in rats^[1].

Parameters	IV (0.2 mg/kg)
t_1/2 (min)	42
CL plasma (mL/min/kg)	37
V_SS (L/kg)	1.6

IC 50

mGluR3: 392 nM (IC₅₀)

References

[1] Engers JL, et al. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. J Med Chem. 2015 Sep 24;58(18):7485-500. DOI:10.1021/acs.jmedchem.5b01005
[2] Max E Joffe, et al. mGlu2 and mGlu3 Negative Allosteric Modulators Divergently Enhance Thalamocortical Transmission and Exert Rapid Antidepressant-like Effects. Neuron. 2020 Jan 8;105(1):46-59.e3. DOI:10.1016/j.neuron.2019.09.044

VU0650786 Preparation Products And Raw materials

Raw materials

Preparation Products

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VU0650786 Suppliers

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VU0650786

Pyrazolo[1,5-a]pyrazin-4(5H)-one, 2-[[(5-chloro-2-pyridinyl)oxy]methyl]-5-(2-fluoro-3-pyridinyl)-6,7-dihydro-7-methyl-, (7R)-

inhibit,anxiolytic activity,antidepressant,Inhibitor,VU-0650786,mGlu3 NAM,VU0650786,mGluR,Metabotropic glutamate receptors,VU 0650786

(7R)-2-{[(5-chloropyridin-2-yl)oxy]methyl}-5-(2-fluoropyridin-3-yl)-7-methyl-4H,5H,6H,7H-pyrazolo[1,5-a]pyrazin-4-one

VU0650786, 10 mM in DMSO

1809085-30-0